Synthesis And Anti-inflammatory Activity Evaluation Of Some Novel 3-amine-6-Alkoxy (Phenoxy)-[1,2,4] Triazolo [3,4,-α] Phthalazine Derivatives | | Posted on:2012-02-10 | Degree:Master | Type:Thesis | | Country:China | Candidate:C Hu | Full Text:PDF | | GTID:2214330338473482 | Subject:Medicinal chemistry | | Abstract/Summary: | PDF Full Text Request | | Starting from phthalic anhydride, several new 3-amine-6-alkoxy(phenoxy)-[1,2,4]triazo-lo[3,4-a]phthalazine derivatives were synthesized as potent anti-inflammatory agent. Their anti-inflammatory activities were studied via the method of the xylene-induced ear edema in mice. The study showed that most of the synthsised compounds exhibited anti-inflammatory activity to a certain extent. Especially, the compounds 6h (3-amine-6-(2-chlorophenoxy)-[1,2, 4]triazolo[3,4-a]phthalazine) and 6s (3-amine6-(4-aminophenoxy)-[1,2,4]triazolo[3,4-a]phth-alazine) showed the highest anti-inflammatory activity (81% and 83% inhibition, respectively, at 0.5 h after i.p. administration) which were slightly more potent than the reference drug Ibuprofen (61%). Furthermore, the structure-activity relationship of these 1,2,4-triazole phthalazines was demonstrated. | | Keywords/Search Tags: | 3-amine-[1,2,4]triazolo[3,4-a]phthalazine, sythesis, mouse ear swelling test, Anti-inflammatory | PDF Full Text Request | Related items |
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